κ-Receptor, together with μ-, δ-, α-, and ORL-1 receptors, belongs to opioid receptor family. μ-Receptor agonist medicine, represented by morphine, has powerful analgesic efficacy, but has many limits in clinical uses due to its side effects, such as dependence and addiction. The central selective κ-receptor agonist not only can be used for analgesic, but also can avoid morphine-like side effects. It can be used for analgesic, antiphlogistic and analgesic, anti-hyperpathia, treating labor pain; used as aquaretic agents, antipruritic; and used for anticonvulsant treatment, anti-hypertension, neural protection, treating HIV infection, and also used in withdrawal of cocaine and morphine addiction. Therefore, selective κ-receptor agonist medicine has good application prospect.